Philanthotoxin 74 features a polyamine-amino acid framework frequently studied as a probe of ion-channel function. The cationic side chains enable strong electrostatic interactions with acidic residues in transmembrane domains. Structural flexibility permits evaluation of binding geometries and conductance modulation. Researchers employ it in neurochemical mechanism studies, ligand-design projects, and structure-activity investigations.
CAT No: R2358
CAS No:1227301-51-0
Synonyms/Alias:Philanthotoxin 74;1227301-51-0;401601-12-5;Philanthotoxin 74 dihydrochloride;PhTx-74 HCl;phtx-74 dihydrochloride;Benzenepropanamide, N-[7-[(4-aminobutyl)amino]heptyl]-4-hydroxy-alpha-[(1-oxobutyl)amino]-, hydrochloride (1:2), (alphaS)-;N-[(2S)-1-[7-(4-aminobutylamino)heptylamino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]butanamide;dihydrochloride;Philanthotoxin 74 (hydrochloride);(S)-N-(1-((7-((4-aminobutyl)amino)heptyl)amino)-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)butyramide dihydrochloride;(S)-N-[7-[(4-Aminobutyl)amino]heptyl]-4-hydroxy-alpha-[(1-oxobutyl)amino]benzenepropanamide dihydrochloride;Philanthotoxin-7,4;C24H42N4O3.2HCl;SCHEMBL2018664;DTXSID50673102;CHEBI:184087;GLXC-04185;HB0499;AKOS024457286;CS-7860;HY-104020A;AS-77383;Benzenepropanamide, N-[7-[(4-aminobutyl)amino]heptyl]-4-hydroxy-a-[(1-oxobutyl)amino]-, hydrochloride (1:2), (aS)-;DA-76820;G13687;N-{7-[(4-Aminobutyl)amino]heptyl}-Nalpha-butanoyl-L-tyrosinamide--hydrogen chloride (1/2);N-[(1S)-1-({7-[(4-AMINOBUTYL)AMINO]HEPTYL}CARBAMOYL)-2-(4-HYDROXYPHENYL)ETHYL]BUTANAMIDE DIHYDROCHLORIDE;
Philanthotoxin 74 is a synthetic analogue of the naturally occurring wasp venom toxin philanthotoxin-433, classified as a polyamine-derived peptide toxin. Its distinctive structure features a polyamine tail linked to an aromatic head group, enabling it to interact selectively with ionotropic glutamate receptors, particularly AMPA, kainate, and NMDA receptor subtypes. Due to its potent antagonistic activity, Philanthotoxin 74 has become a valuable tool in neuropharmacology and synaptic physiology, supporting investigations into excitatory neurotransmission and receptor channel function. Its ability to modulate ion channel activity at the molecular level provides unique opportunities for dissecting the mechanisms of synaptic plasticity, neurotoxicity, and the pharmacology of ligand-gated ion channels.
Electrophysiology research: Philanthotoxin 74 is widely employed in patch-clamp and other electrophysiological studies to probe the functional properties of glutamate receptor channels. By acting as a non-competitive antagonist, it allows researchers to selectively block AMPA and NMDA receptor-mediated currents, thereby facilitating the analysis of receptor subunit composition, channel kinetics, and the contribution of specific receptor populations to synaptic transmission. Its use helps elucidate the biophysical underpinnings of excitatory signaling in central and peripheral nervous system preparations.
Receptor pharmacology: The compound serves as a reference antagonist in the characterization and profiling of ionotropic glutamate receptors. Its selective inhibition of calcium-permeable AMPA and kainate receptors enables detailed assessment of receptor subtype specificity, pharmacological modulation, and structure-activity relationships. Philanthotoxin 74 is instrumental in high-throughput screening assays and ligand-binding studies, supporting the discovery and validation of novel receptor modulators and the mapping of toxin-receptor interaction sites.
Neurotoxicity modeling: In vitro and ex vivo models of excitotoxicity utilize this polyamine toxin to investigate mechanisms underlying neuronal damage caused by excessive glutamate receptor activation. By selectively inhibiting calcium-permeable channels, it provides insight into the role of receptor-mediated calcium influx in neuronal injury, cell death pathways, and neuroprotective strategies. Such studies are critical for advancing the understanding of neurodegenerative processes and synaptic vulnerability.
Synaptic plasticity studies: The ability of Philanthotoxin 74 to modulate postsynaptic receptor function makes it a key reagent in experiments exploring the molecular basis of synaptic plasticity phenomena, including long-term potentiation (LTP) and long-term depression (LTD). Its application allows for the dissection of receptor subtype contributions to synaptic strength changes, helping to clarify the cellular and molecular events that underpin learning and memory at the synaptic level.
Peptide synthesis and analog development: As a structurally defined peptide toxin, Philanthotoxin 74 also serves as a template for the synthesis of novel analogues with tailored pharmacological profiles. Medicinal chemistry and chemical biology laboratories use it as a starting point for the rational design of new polyamine-based channel blockers, aiming to refine selectivity, potency, and pharmacodynamic properties. These efforts expand the toolkit available for probing ion channel function and developing molecular probes for neuroscience research.
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